In recent years, micromolecules with an oxazolidine architecture have been proven to have effects of resisting tumors and inhibiting bacteria, and the potential medical value of the micromolecules with the oxazolidine architecture has been increasing year after year. Besides a method for separating and purifying the micromolecules with the oxazolidine architecture from natural products, in academic aspect, lots of scientists published various methods for synthesizing oxazolidine, and they try to use an artificial synthesizing mode to obtain natural products or novel oxazolidines micromolecules with a curative effect.
For example, an oxazolidinone anti-microbial compound is disclosed in Publication Patent Number 1324603 of the Republic of China, a chemical formula is as shown in the following formula (I). The compound is an anti-microbial agent with special activity, and can be used for resisting Gram-positive human and veterinary pathogens.

Alternatively, in order to obtain an oxazolidinones compound easily, in the aspect of a synthesizing method, an industrial preparation method for an oxazolidinone-2-one derivative, which is disclosed in Publication Patent Number I243168 of the Republic of China, is used for obtaining the oxazolidinone-2-one derivative with the structure as shown in the following formula (II) by using a 1,2-diol derivative which is easily taken from a precursor of a 1,3-dioxolane-2-one derivative as a raw material. Because required steps are fewer when the 1,2-diol derivative which is easily obtained is converted into the oxazolidinone-2-one derivative, the preparation method is efficient; however, the synthesizing method needs to be carried out in the presence of villiaumite.

In addition, synthesis of an isoquinoline oxazolidines compound with a benzene ring on a main architecture can refer to the paper (Ardill, H.; Fontaine, X. L. R.; Grigg, R. Henderson, D.; Montgomery, J.; Sridharan, V.; Surendrakumar, S., Tetrahedron 1990, 46, 6449-6466.) which was published by Grigg in 1990. One equivalent of 1,2,3,4-tetrahydroisoquinoline reacteds with two equivalents of pyridine-2-carboxaldehyde, acetonitrile was used as a solvent to carry out heating reflux for three hours to obtain a 1,3-oxazolidine product as shown in the following formula (III).

The paper (Yamato, M.; Hashigaki, K.; Ishikawa, S.; Qais, N. Tetrahedron Lett., 1988, 29, 6949-6950) which was published by Yamato in 2008 discloses that 2-(2-bromoethyl)-4,5-dimethoxybenzaldehyde is used as an initiator, carries out nucleophilic substitution reaction with (R)-phenylglycinol at first, and then is subjected to intramolecular cyclization reaction under the conditions of alkaline and low temperature to obtain a chiral oxazolidine isoquinoline isomer as shown in the following formula (IV).

Moreover, the paper (Umetsu, K.; Asao, N. Tetrahedron Lett. 2008, 49, 2722-2725.) which was published by Asao in 2008 discloses that an initiator was ortho-vinylbenzaldehyde, after a compound (R)-phenylglycinol is subjected to substitution reaction at first, an intermediate of 2,3-dihydroisoquinoline is then obtained through 6-azaelectrocyclization, and finally intramolecular nucleophilic reaction is carried out to obtain a final product as shown in the following formula (V). An original reaction solvent was converted into dimethyl sulfoxide from 1,4-dioxane.

An existing synthesis method for isoquinoline oxazolidine is not perfect, for example, the synthesis method cannot be carried out at room temperature, or the synthesis method needs to be carried out in the presence of a catalyst, and application and development of the isoquinoline oxazolidines compound are limited. Therefore, a novel synthesis method still needs to be developed with great efforts, and by the novel synthesis method, the isoquinoline oxazolidines compound can be rapidly and efficiently obtained on the premise of not reducing the yield.